Famotidine injections

a technology of famotidine and injection solution, which is applied in the direction of biocide, heterocyclic compound active ingredients, drug compositions, etc., can solve the problems of inability to commercially obtain injection solution and intramuscular administration, limited liquid amount to be administered, and preparation accompanied by vexatious complications, and achieve excellent mixing ability.

Inactive Publication Date: 2006-08-22
ASTELLAS PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention relates to a new method for preparing a stable famotidine injection solution. The method involves using a water-soluble acid amide, such as nicotinic acid amide or isonicotinic acid amide, in combination with an acid substance, such as lactic acid or L-aspartic acid, as a solubilizing agent for famotidine. This approach has not been previously known and offers an effective solution for solubilizing famotidine without using a large amount of non-aqueous solvent or adding a soothing agent. The resulting injection solution has a low viscosity and is stable at room temperature for a long period of time. The invention also provides a new method for increasing the absorbability of famotidine by adding a sugar alcohol or sugar to the injection solution. The use of a water-soluble acid amide as a solubilizing agent for famotidine has not been previously known and offers a new approach for preparing a stable injection solution.

Problems solved by technology

However, an injection solution capable of being preserved at room temperature and capable of being administered intramuscularly is not commercially available.
However, in the case of intramuscular administration, since the administration is physically difficult when a dose is a large amount, the liquid amount to be administered is limited.
However, in general, a freeze-dried preparation should be prepared before use employing a physiologically allowable dissolution liquid such as physiological saline, and thus it can be said that the preparation is a preparation accompanied by vexatious complication.

Method used

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  • Famotidine injections
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Examples

Experimental program
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Effect test

experimental examples

Comparative Formulation 1

Commercially Available Famotidine Injection Preparation (Freeze-dried Preparation)

[0048]The preparation was prepared by reconstituting a commercially available famotidine injection preparation (freeze-dried preparation) with water for injection so that the concentration of famotidine becomes 10 mg / ml.

Comparative Formulation 2

Famotidine Injection Preparation Containing a Water-soluble Non-aqueous Solvent

[0049]In accordance with Example 1 of JP-A-11-193233, an injection solution having formulation of pH 6.4 containing 10 mg / ml of famotidine, 370 mg / ml of polyethylene glycol 400, 20 mg / ml of benzyl alcohol, and 1.8 mg / ml of lactic acid was prepared.

[0050]In this connection, the pH of the injection solution was measured in accordance with the pH measuring method described in General Test Methods of Japanese Pharmacopoeia. The pH of each injection solution of the following Examples was described in each Example.

Experimental Method 1 Measurement of Kinematic Visco...

example 1

10 mg / ml Injection Solution Containing Nicotinic Acid Amide (10%)+Lactic Acid; Containing Benzyl Alcohol

[0083]To 10 g of famotidine and 100 g of nicotinic acid amide were added about 800 ml of water for injection and 19 ml of a 100 mg / ml aqueous lactic acid solution, followed by stirring to dissolve them. After complete dissolution of famotidine, 9 g of benzyl alcohol was added thereto and water for injection was further added to make the total volume 1000 ml, whereby an injection solution having a pH of 6.4 and a kinematic viscosity at room temperature of 1.09 centistokes was obtained.

[0084]After sterile filtration by a usual manner, the solution was charged into an ampoule and after the headspace was replaced with nitrogen, the ampoule was sealed with melting to prepare an injectable product.

example 2

10 mg / ml Injection Solution Containing Nicotinic Acid Amide (5%)+Lactic Acid; Containing Benzyl Alcohol

[0085]To 10 g of famotidine and 50 g of nicotinic acid amide were added about 800 ml of water for injection and 22 ml of a 100 mg / ml aqueous lactic acid solution, followed by stirring to dissolve them. After complete dissolution of famotidine, 9 g of benzyl alcohol was added thereto and water for injection was further added to make the total volume 1000 ml, whereby an injection solution having a pH of 6.2 and a kinematic viscosity at room temperature of 1.00 centistokes was obtained.

[0086]After sterile filtration by a usual manner, the solution was charged into an ampoule and after the headspace was replaced with nitrogen, the ampoule was sealed with melting to prepare an injectable product.

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Abstract

The present invention exhibits a remarkable effect of making it possible to provide a famotidine injection solution containing famotidine at a high concentration, being stable for a long period of time at room temperature, and having a low viscosity without impairing the absorption of famotidine, which can be hardly provided so far.

Description

TECHNICAL FIELD[0001]The present invention relates to an injection solution containing famotidine or its salt. More specifically, the invention relates to a famotidine injection solution containing famotidine or its salt in an amount of about 1 mg / ml to about 40 mg / ml in terms of the base, further containing a water-soluble acid amide in an amount of about 1 mg to about 30 mg per 1 mg of famotidine, and an acidic substance and having a pH of about 5.5 to about 7.5 and a kinematic viscosity at room temperature of about 0.9 centistokes or more to about 3 centistokes or less.BACKGROUND ART[0002]Famotidine is a pharmaceutical agent excellent in inhibitory action of gastric acid secretion based on a histamine H2-receptor antagonistic action and generally used in the form of an oral or injection preparation as an agent for treating gastric ulcer, duodenal ulcer, and other digestive diseases (cf. Merck Index thirteen edition, page 696 and so on). With regard to famotidine injection prepara...

Claims

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Application Information

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Patent Type & AuthorityPatents(United States)
IPC IPC(8): A61K9/00A61K31/426A61K47/00A61K47/10A61K47/12A61K47/18A61K47/22A61K47/26A61P1/04
CPCA61K9/0019A61K31/426A61K47/18A61K47/12A61K47/10A61K47/26A61K47/183A61K47/22A61P1/04A61K9/08
InventorNAKATA, KATSUNORIYATABE, HIROSHINISHIKAWAHARA, TSUKASA
OwnerASTELLAS PHARMA INC